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Netarsudil and latanoprost: Drug information

Netarsudil and latanoprost: Drug information
(For additional information see "Netarsudil and latanoprost: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Rocklatan
Pharmacologic Category
  • Ophthalmic Agent, Antiglaucoma;
  • Prostaglandin, Ophthalmic;
  • Rho Kinase Inhibitor
Dosing: Adult
Elevated intraocular pressure

Elevated intraocular pressure: Ophthalmic: One drop in the affected eye(s) once daily in the evening (maximum: 1 drop in affected eye(s) once daily).

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in manufacturer's labeling. However, dosage adjustment unlikely due to low systemic absorption.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in manufacturer's labeling. However, dosage adjustment unlikely due to low systemic absorption.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. See individual agents.

>10%:

Local: Application site pain (20%)

Ophthalmic: Conjunctival hyperemia (59%), epithelial keratopathy (15%), conjunctival hemorrhage (11%)

1% to 10%: Ophthalmic: Blurred vision (5% to 8%), decreased visual acuity (5% to 8%), eye discomfort (5% to 8%), eye pruritus (5% to 8%), increased lacrimation (5% to 8%)

Contraindications

There are no contraindications listed in the manufacturer's labeling.

Warnings/Precautions

Concerns related to adverse effects:

• Bacterial keratitis: Inadvertent contamination of multiple-dose ophthalmic solutions has caused bacterial keratitis.

• Ocular effects: May change/increase brown pigmentation of the iris, the eyelid skin, and eyelashes; length and/or number of eyelashes may also be increased. Pigmentation of the iris is likely to be permanent although iris color change may not be noticeable for months to years; pigmentation of the periorbital tissue and eyelash changes may be reversible following discontinuation of therapy. Long-term consequences and potential injury to eye are not known.

• Ocular inflammation: Intraocular inflammation and exacerbation of inflammation may occur; use with caution in patients with a history of intraocular inflammation (eg, iritis/uveitis) and generally avoid use in patients with active intraocular inflammation.

Disease-related concerns:

• Herpetic keratitis: Use with caution in patients with a history of herpes simplex keratitis; reactivation may occur. Avoid use in patients with active herpes simplex keratitis.

• Ocular disease: Use with caution in aphakic patients, pseudophakic patients with a torn posterior lens capsule, or patients with risk factors for macular edema. Safety and efficacy have not been determined for use in patients with angle-closure, inflammatory, or neovascular glaucoma.

Special populations:

• Contact lens wearers: Solution contains benzalkonium chloride which may be absorbed by contact lenses. Remove contacts prior to administration and wait 15 minutes before reinserting.

Other warnings/precautions:

• Appropriate use: Avoid concurrent use of 2 or more prostaglandins or prostaglandin analogs or more frequent administration than once daily; may decrease the IOP lowering effect or cause paradoxical elevations in IOP.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Ophthalmic:

Rocklatan: Netarsudil dimesylate 0.02% and latanoprost 0.005% (2.5 mL) [contains benzalkonium chloride]

Generic Equivalent Available: US

No

Pricing: US

Solution (Rocklatan Ophthalmic)

0.02-0.005% (per mL): $164.78

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

Ophthalmic: May be used with other eye drops to lower IOP. If more than one topical ophthalmic drug is being used, administer the drugs at least 5 minutes apart. Remove contact lenses prior to administration and wait 15 minutes before reinserting. Avoid touching the dropper tip with fingers, eyes, eyelids, or surrounding areas to minimize contamination of the dropper tip.

Use: Labeled Indications

Elevated intraocular pressure: Reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Nonsteroidal Anti-Inflammatory Agents: May diminish the therapeutic effect of Prostaglandins (Ophthalmic). Nonsteroidal Anti-Inflammatory Agents may also enhance the therapeutic effects of Prostaglandins (Ophthalmic). Risk C: Monitor therapy

Nonsteroidal Anti-Inflammatory Agents (Ophthalmic): May diminish the therapeutic effect of Prostaglandins (Ophthalmic). Nonsteroidal Anti-Inflammatory Agents (Ophthalmic) may enhance the therapeutic effect of Prostaglandins (Ophthalmic). Risk C: Monitor therapy

Prostaglandins (Ophthalmic): The concomitant use of Prostaglandins (Ophthalmic) and Latanoprost may result in increased intraocular pressure. Risk X: Avoid combination

Pregnancy Considerations

Systemic absorption is limited following ophthalmic application.

If ophthalmic agents are needed during pregnancy, the minimum effective dose should be used in combination with punctal occlusion to decrease potential exposure to the fetus (Samples 1988). Also refer to individual monographs.

Breastfeeding Considerations

It is not known if netarsudil or latanoprost are present in breast milk; however, systemic absorption is limited following ophthalmic application.

According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother. Also refer to individual monographs.

Monitoring Parameters

Monitor IOP; regularly examine patients who develop increased iris pigmentation.

Mechanism of Action

Although the exact mechanism is unknown, netarsudil is a Rho kinase inhibitor and latanoprost is a prostaglandin F2-alpha analog, and both may reduce intraocular pressure by increasing the outflow of aqueous humor.

Pharmacokinetics (Adult Data Unless Noted)

Absorption: Limited. Latanoprost is absorbed through the cornea and hydrolyzed to the biologically active acid (measurable in the aqueous humor during the first 4 hours and in the plasma during the first hour).

Distribution: Latanoprost: Vd: 0.16 ± 0.02 L/kg

Metabolism:

Latanoprost: Isopropyl ester prodrug is hydrolyzed to the biologically active acid in the cornea. Biologically active acid reaching systemic circulation is primarily metabolized hepatically via fatty acid beta-oxidation.

Netarsudil: Metabolized by ophthalmic esterases to active metabolite, AR-13503.

Half-life elimination: Latanoprost: 17 minutes

Excretion: Latanoprost: Urine: ~88% (as metabolites)

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (DE) Germany: Roclanda;
  • (IE) Ireland: Roclanda;
  • (PR) Puerto Rico: Rocklatan
  1. Rocklatan (netarsudil/latanoprost) [prescribing information]. Irvine, CA: Aerie Pharmaceuticals Inc; June 2020.
  2. Samples JR, Meyer SM. Use of ophthalmic medications in pregnant and nursing women. Am J Ophthalmol. 1988;106(5):616-623. [PubMed 2903673]
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